Hypnotics for insomnia

Diazepam is used for the control of anxiety and tension, the relief of muscle spasms, and the management of acute agitation during alcohol withdrawal, but it itself may be habit-forming. Chlordiazepoxide has similar uses and its synthesis is somewhat analogous to diazepam. Flurazepam is a hypnotic, useful for insomnia treatment. It is reported to provide 7-8 hr of restful sleep. 

The sedative-hypnotic action of chloral hydrate should be explained by the formation of trichloroethanol, which is synthesized as a result of its reduction in tissues. Despite the fact that the precise mechanism of action of chloral hydrate is not known, it evidently acts analogous to ethanol on the CNS by inCTeasing membrane permeability, which leads to sedation or sleep. Chloral hydrate can be used for insomnia as an alternative to benzodiazepines. Synonyms for this drug are aquachloral, chloradorm, chloratol, noctec, and others. 

Zaleplon (Sonata) [C IV] [Sedotive/Hypnotic] Uses Insomnia Action A nonbenzodiazepine sedative/hypnotic, a pyrazolopyrimidine Dose 5-20 mg hs PRN -1- w/ renal/hepatic insuff, elderly Caution [C, /-] w/ mental/ psychological conditions Contra Component allergy Disp Caps SE HA, edema, amnesia, somnolence, photosens Interactions t CNS depression W/ CNS d es-sants, imipramine, thioridazine, EtOH X effects W/ carbamazepine, phenobarbital, phenytoin, rifampin EMS Concurrent EtOH can t adverse CNS effects OD May cause profound CNS depression symptomatic and supportive Zanamivir (Relenza) [Antiviral/Neuramidase Inhibitor] Uses Influenza A (including HlNl swine flu) B Action X Viral neuraminidase Dose Adults Feds > 7 y.2 inhal (10 mg) bid for 5 d initiate w/in 48 h of Sxs Caution [C, M] Contra Pulm Dz Disp Powder for inhal SE Bron-chospasm, HA, GI upset EMS Does not reduce risk of transmitting virus monitor for bronchospasm or other severe resp events OD May cause resp problems s5rmptomatic and supportive... 

Although benzodiazepines, zolpidem, zaleplon, and eszopiclone are the mainstay of pharmacotherapy for insomnia, other sedating drugs, such as trazodone, diphenhydramine, or chloral hydrate, also may be used. Insomnia should first be addressed diagnostically, and in most cases, nonpharmacological interventions should be attempted before treatment with a hypnotic is instituted. Hypnotic agents should be administered in the lowest effective dose. Medications commonly prescribed for insomnia, along with their recom-... 

Because insomnia is often transient and intermittent, the prolonged administration of estazolam is generally neither necessary nor recommended. Caution should be exercised in prescribing this hypnotic for elderly or debilitated patients, as well as for those with impaired renal or hepatic function, because of increased sensitivity or reduced capacity to metabolize and eliminate the drug. The recommended initial dose is 1 mg, but some may need a 2 mg dose. For the elderly, a 0.5 or 1 mg dose is appropriate. 

This newest non-BZD hypnotic is a pyrazolopyrimidine derivative with a fuii agonist activity on centrai BZD receptors B2 type. It is an effective hypnotic for the short-term treatment of insomnia. Because of its very short half-life (almost an hour), it may be useful for patients experiencing difficulty falling asleep and in those who wake up at night and who have trouble falling back to sleep. Zaleplon is rapidly absorbed after oral administration and its mean, apparent elimination half-life is similar to that obtained after i.v. infusion. Zaleplon is extensively metabolized in the liver by aldehyde oxidase, and to a lesser extent by CYP3A4. This drug is excreted in the urine (156). 

DeClerck A, Smits M. Zolpidem, a valuable alternative to benzodiazepine hypnotics for chronic insomnia. J Int Med Res 1999 27 253-263. 

When these issues are taken into consideration, there is still a high frequency of primary insomnia, as well as secondary insomnia the primary cause of which cannot be satisfactorily treated. Many patients also have both a psychiatric disorder and a primary insomnia. Still others have a psychiatric disorder requiring a sleep-disrupting antidepressant. Here we will discuss the use of sedative-hypnotics for these patients. 

The newer sedative-hypnotics that are not benzodiazepines are rapidly becoming the first-line treatment for insomnia. These agents not only have pharmacodynamic advantages over benzodiazepines in terms of their mechanism of action, but perhaps more importantly, pharmacokinetic advantages as well. Three nonbenzodiazepine sedative-hypnotic agents that are now available are zaleplon (a pyrazolopyrimidine), zopiclone (a cyclopyrrolone not available in the United States), and zolpidem (an imidazopyridine) (Figs. 8—28-8—30 Table 8—4). 

Longer-term difficulties associated with benzodiazepine use for insomnia come from observations that many patients develop tolerance for these agents, so that they stop working after a week or two. To avoid this, patients must take a sleeping pill only a few times within several days, or for only about 10 days in a row followed by several days or weeks with no drug treatment. Furthermore, if patients persist in taking benzodiazepines as sedative-hypnotics for several weeks to months, there can be a withdrawal syndrome once the medications are stopped, particularly if they are stopped suddenly. This is discussed in further detail in Chapter 13. 

The nonbenzodiazepine sedative-hypnotics zaleplon, zolpidem, and zopiclone are replacing benzodiazepine sedative-hypnotics as first-line treatments for insomnia. Some antidepressants, such as sedating tricyclic antidepressants and trazodone, are also used as sedative-hypnotic agents for the treatment of insomnia. 

To review the drug treatments for insomnia, including newer nonbenzodiazepine hypnotics as well as benzodiazepine and other hypnotics. 

The time spent reviewing sedative hypnotics for the treatment of insomnia was just right. ... 

Morgan K, Dixon S, Mathers N, et al. Psychological treatment for insomnia in the regulation of long-term hypnotic drag use. Health Technol Assess. 2004 8 ... 

Lady s slipper is believed to have sedative, mild hypnotic, antispasmodic, and thymoleptic properties. Traditionally, it has been used for insomnia, hysteria, emotional tension, anxiety states, and specifically for anxiety states with insomnia. 

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